title: Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery.
abstract: Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (<1000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.
authors.affiliation: Asian Institute of Medicine Science and Technology, Semeling , Bedong , Malaysia .
authors.forename: B Sajeev
authors.initials: BS
authors.lastname: Kumar
authors.forename: R
authors.initials: R
authors.lastname: Saraswathi
authors.forename: K Venkates
authors.initials: KV
authors.lastname: Kumar
authors.forename: S K
authors.initials: SK
authors.lastname: Jha
authors.forename: D P
authors.initials: DP
authors.lastname: Venkates
authors.forename: S A
authors.initials: SA
authors.lastname: Dhanaraj
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D004337:Drug Carriers; D004355:Drug Stability; D005905:Glyburide / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D054709:Lecithins / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D036103:Nanotechnology; D010179:Pancreas / Q000378:metabolism; D010316:Particle Size; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D033362:Powder Diffraction; D017208:Rats, Wistar; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D004337:Drug Carriers; D007004:Hypoglycemic Agents; D054709:Lecithins; D011136:Polysorbates; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D005905:Glyburide